Formulation: A solid
Formal Name: 2-[1-[(1R)-1-(2,6-dichloro-3-cyclopropylphenyl)ethyl]-1H-imidazo[4,5-c]pyridin-6-yl]-αR-methyl-benzeneacetic acid
Purity: ≥98%
Formula Markup: C26H23Cl2N3O2
Formula Weight: 480,4
Shelf life (days): 1460
CAS Number: 2764704-18-7
Notes: LSN3318839 is a positive allosteric modulator (PAM) of glucagon-like peptide 1 receptor (GLP-1R).{67807} It potentiates increases in cAMP accumulation induced by the GLP-1R full agonist GLP-1 (9-36), but not the GLP-1R partial agonist GLP-1 (7-36), in INS-1 832/3 cells. LSN3318839 (1 and 3 µM) increases insulin levels in the presence, but not absence, of GLP-1 (9-36) in INS-1 832/3 cells under high-glucose conditions. It reduces blood glucose levels in glucose-dependent insulinotropic polypeptide receptor (GIPR) knockout mice in an oral glucose tolerance test when administered at a dose of 30 mg/kg and has an additive effect on reducing blood glucose levels in GIPR knockout mice when administered at 10 or 30 mg/kg in combination with the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin.
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